Tag: retinoid

There is much confusion over the range of retinoids available and the meaning of the strength and percentages on product labels. And some manufacturers use this to deliberately mislead consumers…more below

There are a few nutrients that skin really needs and vitamin A is definitely one of them. Whether you get it from your diet, or in a topical cream, the protective and nourishing properties of A, and the nutrients your body uses to make it, lend a hand in keeping skin healthy, firm and radiant.

Unlike many other nutrients, vitamin A is a group of compounds that includes its active forms (retinal, retinol and retinoic acid) and other provitamin A carotenoids, like beta-carotene. Beta-carotene is the form of vitamin A that we get directly from the plant foods we eat. Pre-formed, or active forms, are found in animal foods and beta-carotene is converted into the retinol form of vitamin A, inside our bodies.

The first retinoid (tretinoin) was originally FDA approved in 1962 and developed as a powerful prescription acne treatment in the late 1960s. It appeared to work by reducing the ability of the epithelial cells in the hair follicles to stick together, and make the cells divide faster – increasing cell turnover in the outer layers of skin. For patients with acne, this decreased the build-up of keratin which formed blackheads, and improved the health of the skin.

Vitamin A has a wider range of uses because it targets several skin health issues. Dermatologists noticed that patients using tretinoin experienced not just clearer but softer, brighter, skin with less superficial lines. Today there are three prescription-strength retinoids: tretinoin (brands include Atralin, Avita, Retin-A, Renova), tazarotene (Avage, Tazorac, fabior), and adapalene (Differin).

What happens when you feed your body vitamin A

• It protects against UV damage and slows extrinsic aging

Most of your vitamin A intake comes from eating foods rich in beta-carotene and provitamin A carotenoids, which are potent anti-oxidants. Not only do these quench the free radicals that break down collagen and contribute to fine lines and sagging skin, they also lessen skin’s sensitivity to the sun, providing some natural protection against sun-induced redness and pigmentation.

• It protects against infection and boosts immunity

Vitamin A is important for resistance to infection and a healthy immune system, so a vitamin A deficiency can lead to death from respiratory and other infections. Vitamin A plays a vital role in maintaining your body’s natural defenses, including the mucous barriers in your eyes, lungs, gut and genitals which help trap bacteria and other infectious agents.

It is also involved in the production and function of white blood cells, which help capture and clear bacteria and other pathogens from your bloodstream. This means that a deficiency in vitamin A can increase your susceptibility to infections and delay your recovery when you get sick. In fact, in countries where infections like measles and malaria are common, correcting vitamin A deficiency in children has been shown to decrease the risk of dying from these diseases.

Your skin is the body’s largest organ and an important part of your immune system – your first line of defense against bacteria, pollutants and infection. By promoting keratinocyte turnover in the epidermis, vitamin A helps strengthen the natural lipid barrier, protecting your skin from harmful irritants that attempt to attack the surface.

• It increases cellular turnover

Retinal, retinol and retinoic acid are important to cell production and growth. Vitamin A thickens and stimulates the dermis, the deeper level of the skin where your collagen, elastin and blood vessels reside. This means it aids blood circulation to the surface of the skin and supports the renewal of skin cells. Vitamin A increases the deposition of collagen and slows the normal aging breakdown of collagen and elastin. Because vitamin A and carotenoids play such a big role in cell and tissue growth, not getting enough can lead to weak, fragile skin, causing problems ranging from dryness, to wounds that heal slower.

• Protects your vision

Vitamin A helps protect the cornea and it is essential for good vision. A vitamin A deficiency causes damage to the retina, which contributes to blindness. When used in combination with other antioxidant vitamins, it also appears to play a role in decreasing the risk of vision loss from macular degeneration.

• May lower the risk of certain cancers

In observational studies, eating higher amounts of vitamin A in the form of beta-carotene has been linked to a decreased risk of certain types of cancer, including Hodgkin’s lymphoma, as well as cervical, lung and bladder cancer.

How much should you get?

Vitamin A that comes from animal food sources is not water-soluble and therefore is not readily excreted from the body. Instead, it is stored in body fat and, if ingested in excess amounts, can build up in the body and become toxic.

Beta-carotene and other provitamin A carotenoids found in fruits and vegetables don’t pose the same vitamin A toxicity risk. These compounds are water-soluble and are easily eliminated from the body, so vitamin A toxicity from vegetarian food sources is rare.

Beta-carotene supplements, however, may have serious risks for smokers. Two studies have found that smokers taking daily supplements containing 20 to 30 mg of beta-carotene had an increased risk of lung cancer compared with smokers who did not take supplements.

The recommended daily amount of vitamin A is 900 micrograms (ug) for adult men and 700 ug for adult women.

Retinoids can be found in animal products, such as:

• salmon
• beef liver (the highest level!)
• dairy products, such as milk, butter, and cheddar cheese
• eggs
• fish
• cod liver oil
• prawns

Carotenoids can be found in plant products, such as:

• carrots (the highest level!)
• tomatoes
• sweet potatoes
• leafy green vegetables
• fruits, such as mango, apricots, and plums.

Taking more than 10,000 ug a day of oral vitamin A supplements long term can cause:

• Bone thinning
• Liver damage
• Headaches
• Diarrhea
• Nausea
• Skin irritation
• Pain in the joints and bone
• Birth defects

The oral acne drug, Accutane (isotretinoin), can be dangerous. It may cause serious side-effects, most notably birth defects. But Accutane is also one of the most effective prescription drugs available for severe acne.

The oral drug Accutane may cause serious side-effects, most notably birth defects

Why topical vitamin A is better

• It smoothes wrinkles

Topical vitamin A’s are proven wrinkle-fighters and many dermatologists’ go-to active for anti-aging. Research has shown that these ingredients are able to stimulate collagen production and lessen the effect of the enzymes that degrade it. Retinoids “turn on” fibroblasts to make new collagen, strengthen your skin and fill in fine lines below the surface, so the skin looks smoother.

• It evens skin tone

Vitamin A creams can help lighten sun-induced brown spots and boost skin radiance in two ways – firstly, by increasing and normalising skin cell turnover, which helps shed pigmented and damaged surface cells, making room for healthier cells. Secondly, retinoids block the enzyme needed for melanin (pigment) production, tyrosinase, further helping to deliver an even-toned, glowing skin.

• It clears acne

Pimples form when pores become clogged with dead skin cells, bacteria and oil, providing the perfect breeding ground for P.acnes, a common bacteria responsible for blemishes. When vitamin A creams stimulate cell turnover the same process happens within the pores themselves, helping to slow oil production and keep pores clear.

But…not all retinoids are created equal

There is much confusion over the range of retinoids available and the meaning of the strength and percentages on product labels. And some manufacturers use this to deliberately mislead consumers (see my additional footnote at the end of this blog for more).

‘Retinoid’ is the generic term for the family of ingredients related to Vitamin A which occur naturally in our bodies. When referring to topically applied retinoids, the only two retinoids that your skin is able to process immediately (ie that cell receptors recognise) are retinoic acid and hydroxypinacolone retinoate (the form we use). All other forms of retinoids have to be converted by skin enzymes into retinoic acid before the skin is able to use them.

In reality you would need a 20% concentration of retinol to equal 0.05% tretinoin prescription strength retinoic acid, or the 1% hydroxypinacolone retinoate we use

These are the main forms of retinoids used in topical skincare products:

• Retinol

Retinol is a specific form of vitamin A that is naturally produced in your body. It is often used in over the counter products since it is inexpensive. Non-medical grade Retinol is typically sold in products at the 1% or 2% level, but some products use up to 5%. Don’t confuse this with the 0.05% retinoic acid in tretinoin (or the 1% hydroxypinacolone retinoate we use in Retinic A10). In reality you would need a 20% concentration of retinol to equal 0.05% tretinoin prescription strength retinoic acid, or the 1% hydroxypinacolone retinoate we use.

When applied to your skin, enzymes in your skin convert retinol into retinaldehyde and then into retinoic acid, in a two-part conversion process. The conversion into retinoic acid can take a few days, sometimes weeks, which is why you should use retinol products consistently for a few months before expecting to see results. Count on twelve weeks before seeing results. During this time, much of what you applied will never convert to the active form, since retinol is extremely sensitive to degradation, especially as induced by light.

• Retinyl palmitate

is the ester of retinol combined with palmitic acid, a saturated fatty acid and a major component of palm oil. Although it absorbs skin better than retinol, it is much weaker, since it must first be converted to retinol before the further conversion steps to retinoic acid can occur. It is therefore somewhat gentler on the skin but the trade-off is efficacy.

• Retinaldehyde

Also powerful and effective is Retinaldehyde – it has the advantage of having no burn, and also being available without prescription. The disadvantage is that it is expensive when added to skincare products.

• Retinoic Acid

Medical grade tretinoin, available on prescription only, and you need to develop a tolerance to it since it can burn, itch, scale and peel. Retinoic acid is powerful at the level of 0.05% (brands include Retin-A). Retinoic acid can be used by your skin without having to be converted by skin enzymes. This makes it about 100 times more potent than the average over-the-counter products containing pure retinol. It is used mainly as a prescription drug for severe acne, although some dermatologists prescribe it for patients in a hurry to renew ageing skin and who are willing to tolerate the side-effects.

Our form of retinoid leapfrogs all the others

We were the first company in SA to use a new generation of retinoid, called hydroxypinacolone retinoate, in skincare products. This form of retinoid in unique in that, like retinoic acid, it is able to bind directly to retinoid receptors, without needing to undergo enzymatic conversion. As such, its residence time in the skin is lower, since it is able to get to work straight away.  Thanks to our transdermal technology, it is able to penetrate quicker, lowering the irritation factor and potential for inflammatory responses.

So, the order of strengths of the different retinoids, from weakest to strongest, is:

retinyl palmitate < retinol < retinaldehyde < hydroxypinacolone retinoate < retinoic acid < isotretinoin

Try a good retinoid on your skin. It may take weeks but you WILL see a difference!

Update on 14-09-18:

We had an excellent question from Maryanne (below) concerning Granactive Retinoid. I believe some manufacturers are deliberately misleading consumers with the way they state the concentration of this retinoid. See my answer to her comment below.